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Edmund Cheung So et al.
European journal of pharmacology, 879, 173141-173141 (2020-05-01)
Dapagliflozin (DAPA) or canagliflozin (CANA), Na+-dependent glucose co-transporter type 2 (SGLT2) inhibitors, were used for treatment of type II diabetes mellitus. Addition of DAPA or CANA suppressed M-type K+ current (IK(M)) in pituitary tumor (GH3) and pheochromocytoma PC12 cells. The IC50
D Guan et al.
Journal of neurophysiology, 106(4), 1722-1733 (2011-06-24)
After block of Kv1- and Kv2-mediated K(+) currents in acutely dissociated neocortical pyramidal neurons from layers II/III of rat somatosensory and motor cortex, the remaining current is slowly activating and persistent. We used whole cell voltage clamp to show that
Jin Ryeol An et al.
Journal of applied toxicology : JAT, 40(9), 1297-1305 (2020-04-15)
Iloperidone, a second-generation atypical antipsychotic drug, is widely used in the treatment of schizophrenia. However, the side-effects of iloperidone on vascular K+ channels remain to be determined. Therefore, we explored the effect of iloperidone on voltage-dependent K+ (Kv) channels in
Mohamed Kreir et al.
European journal of pharmacology, 858, 172474-172474 (2019-06-27)
The Kv7 family of voltage-dependent non-inactivating potassium channels is composed of five members, of which four are expressed in the CNS. Kv7.2, 7.3 and 7.5 are responsible for the M-current, which plays a critical role in the regulation of neuronal
Jin Ryeol An et al.
Biochemical and biophysical research communications, 529(2), 191-197 (2020-07-25)
We investigated the effect of ziprasidone, a widely used treatment for schizophrenia, on voltage-dependent K+ (Kv) channels of coronary arterial smooth muscle cells using the patch-clamp technique. Ziprasidone dose-dependently inhibited Kv channels with an IC50 value of 0.39 ± 0.06 μM and a
Allan Kjeldsen Hansen et al.
Journal of neurophysiology, 112(3), 631-643 (2014-09-25)
Behavior-associated theta-frequency oscillation in the hippocampal network involves a patterned activation of place cells in the CA1, which can be accounted for by a somatic-dendritic interference model predicting the existence of an intrinsic dendritic oscillator. Here we describe an intrinsic
Ke-Tao Ma et al.
Hearing research, 239(1-2), 20-33 (2008-03-04)
Adequate cochlear blood supply by the spiral modiolar artery (SMA) is critical for normal hearing. ACh may play a role in neuroregulation of the SMA but several key issues including its membrane action mechanisms remain poorly understood. Besides its well-known
Olga Zavaritskaya et al.
Hypertension (Dallas, Tex. : 1979), 61(1), 151-159 (2012-11-28)
KCNQ channels have been identified in arterial smooth muscle. However, their role in vasoregulation and chronic vascular diseases remains elusive. We tested the hypothesis that KCNQ channels contribute to periadventitial vasoregulation in peripheral skeletal muscle arteries by perivascular adipose tissue
Bikash R Pattnaik et al.
American journal of physiology. Cell physiology, 302(5), C821-C833 (2011-12-03)
Recently, we demonstrated the expression of KCNQ1, KCNQ4, and KCNQ5 transcripts in monkey retinal pigment epithelium (RPE) and showed that the M-type current in RPE cells is blocked by the specific KCNQ channel blocker XE991. Using patch-clamp electrophysiology, we investigated
Motoharu Yoshida et al.
Journal of neurophysiology, 98(5), 2779-2794 (2007-08-31)
The M-current (current through Kv7 channels) is a low-threshold noninactivating potassium current that is suppressed by muscarinic agonists. Recent studies have shown its role in spike burst generation and intrinsic subthreshold theta resonance, both of which are important for memory
Elisa Martelletti et al.
Frontiers in cellular neuroscience, 14, 561857-561857 (2020-10-27)
Progressive hearing loss is very common in the human population but we know little about the underlying molecular mechanisms. Synaptojanin2 (Synj2) has been reported to be involved, as a mouse mutation led to a progressive increase in auditory thresholds with
Caroline S Hirst et al.
PloS one, 10(3), e0123436-e0123436 (2015-03-24)
The enteric nervous system arises from neural crest-derived cells (ENCCs) that migrate caudally along the embryonic gut. The expression of ion channels by ENCCs in embryonic mice was investigated using a PCR-based array, RT-PCR and immunohistochemistry. Many ion channels, including
Microwave-assisted rapid synthesis of neurotransmitter release enhancer linopiridine and its new analogues
Yadav JS and Reddy BVS
Synthetic Communications, 33(18), 3115-3121 (2003)
Iain A Greenwood et al.
Frontiers in physiology, 10, 1573-1573 (2020-01-30)
Within the vasculature Kv7 channels are key regulators of basal tone and contribute to a variety of receptor mediated vasorelaxants. The Kv7.4 isoform, abundant within the vasculature, is key to these processes and was recently shown to have an obligatory
Mi Seon Seo et al.
Toxicology and applied pharmacology, 403, 115153-115153 (2020-07-28)
We investigated the vasodilatory effects of empagliflozin (a sodium-glucose co-transporter 2 inhibitor) and the underlying mechanisms using rabbit aorta. Empagliflozin induced vasodilation in a concentration-dependent manner independently of the endothelium. Likewise, pretreatment with the nitric oxide synthase inhibitor L-NAME or
Alana Firl et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 35(4), 1675-1686 (2015-01-30)
Spontaneous retinal activity mediated by glutamatergic neurotransmission-so-called "Stage 3" retinal waves-drives anti-correlated spiking in ON and OFF RGCs during the second week of postnatal development of the mouse. In the mature retina, the activity of a retinal interneuron called the
Jing-Yi Jeng et al.
The Journal of physiology, 598(19), 4339-4355 (2020-07-28)
Age-related hearing loss (ARHL) is associated with the loss of inner hair cell (IHC) ribbon synapses, lower hearing sensitivity and decreased ability to understand speech, especially in a noisy environment. Little is known about the age-related physiological and morphological changes
Pernille Elmedyb et al.
Basic & clinical pharmacology & toxicology, 100(5), 316-322 (2007-04-24)
In neuronal tissue, KCNQ2-5 channels conduct the physiologically important M-current. In some neurones, the M-current may in addition be conducted partly by ERG potassium channels, which have widely overlapping expression with the KCNQ channel subunits. XE991 and linopiridine are known
S W Tam et al.
Advances in experimental medicine and biology, 363, 47-56 (1995-01-01)
Linopirdine (DuP 996, AVIVA), currently in Phase III clinical trial for the treatment of Alzheimer's disease, is a representative of a class of novel molecules which enhances the stimulus-evoked but not basal release of several neurotransmitters including ACh, DA, 5-HT
Anastasia A Shvetsova et al.
Acta physiologica (Oxford, England), 225(2), e13176-e13176 (2018-08-24)
Potassium channels are key regulators of smooth muscle membrane potential and arterial tone. However, the roles of potassium channels in vascular tone regulation in the systemic circulation during early postnatal development are poorly understood. Therefore, this study tested the hypothesis
Tzu-rong Su et al.
Acta pharmacologica Sinica, 30(9), 1220-1226 (2009-08-25)
KCNQ4 channels play an important part in adjusting the function of cochlear outer hair cells. The aim of this study was to investigate the effects of ser/thr phosphatase inhibitors on human KCNQ4 channels expressed in Xenopuslaevis oocytes. Synthetic cRNA encoding
Geoffrey W Abbott et al.
Journal of vascular research, 53(3-4), 138-148 (2016-10-07)
Voltage-gated potassium (Kv) channels formed by Kv7 (KCNQ) α-subunits are recognized as crucial for vascular smooth muscle function, in addition to their established roles in the heart (Kv7.1) and the brain (Kv7.2-5). In vivo, Kv7 α-subunits are often regulated by
Jin Ryeol An et al.
Acta biochimica et biophysica Sinica, 52(3), 320-327 (2020-02-16)
In this study, we explore the inhibitory effects of protriptyline, a tricyclic antidepressant drug, on voltage-dependent K+ (Kv) channels of rabbit coronary arterial smooth muscle cells using a whole-cell patch clamp technique. Protriptyline inhibited the vascular Kv current in a
Sonia Cavaliere et al.
PloS one, 6(9), e23898-e23898 (2011-09-15)
Of the five human KCNQ (Kv7) channels, KCNQ1 with auxiliary subunit KCNE1 mediates the native cardiac I(Ks) current with mutations causing short and long QT cardiac arrhythmias. KCNQ4 mutations cause deafness. KCNQ2/3 channels form the native M-current controlling excitability of
Jin Ryeol An et al.
European journal of pharmacology, 874, 173027-173027 (2020-02-23)
We evaluated the inhibitory effects of the atypical antipsychotic drug risperidone on voltage-dependent K+ (Kv) channels in rabbit coronary arterial smooth muscle cells. Risperidone suppressed Kv currents in reversible and concentration-dependent manners with an apparent half-maximal effective concentration (IC50 value)
Chin-Wei Huang et al.
The international journal of neuropsychopharmacology, 11(5), 597-610 (2008-01-11)
Oxcarbazepine (OXC), one of the newer anti-epileptic drugs, has been demonstrating its efficacy on wide-spectrum neuropsychiatric disorders. However, the ionic mechanism of OXC actions in neurons remains incompletely understood. With the aid of patch-clamp technology, we first investigated the effects
S Y M Yeung et al.
British journal of pharmacology, 151(6), 758-770 (2007-05-24)
This study represents a novel characterisation of KCNQ-encoded potassium channels in the vasculature using a variety of pharmacological and molecular tools to determine their role in contractility. Reverse transcriptase polymerase chain reaction (RT-PCR) experiments were undertaken on RNA isolated from
Calvin Wu et al.
European journal of pharmacology, 667(1-3), 188-194 (2011-07-02)
Tinnitus affects approximately 50 million people in the USA alone, with 10 million being highly debilitated. Pharmacotherapy for tinnitus is still in emerging stages due to time consuming clinical trials and/or animal experiments. We tested a new cellular model where
Xin Zhou et al.
Experimental neurology, 229(2), 471-483 (2011-04-07)
Voltage-gated K(+) channels are key regulators of neuronal excitability, playing major roles in setting resting membrane potential, repolarizing the cell membrane after action potentials and affecting transmitter release. The M-type channel or M-channel is a unique voltage- and ligand-regulated K(+)
Manuela Cerina et al.
British journal of pharmacology, 172(12), 3126-3140 (2015-02-17)
The existence of functional K(v)7 channels in thalamocortical (TC) relay neurons and the effects of the K(+)-current termed M-current (I(M)) on thalamic signal processing have long been debated. Immunocytochemical evidence suggests their presence in this brain region. Therefore, we aimed
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